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SML2133

Sigma-Aldrich

Ro 65-6570 Hydrochloride

≥98% (HPLC)

Synonym(s):

(RS)-8-(1,2-Dihydro-1-acenaphthylenyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one Hydrochloride, (RS)-8-Acenaphthen-1-yl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one hydrochloride, Ro65-6570 Hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C25H25N3O · HCl
CAS Number:
228246-34-2
Molecular Weight:
419.95
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C1NCN(C2=CC=CC=C2)C13CCN(C4CC5=C6C4=CC=CC6=CC=C5)CC3.Cl

Biochem/physiol Actions

Ro 65-6570 is a nonpeptidic, high-affinity (Ki = 0.52 against 0.1 nM OFQ for binding human ORL1) nociceptin/orphanin FQ (N/OFQ) receptor ORL-1 (KOR-3, NOP) agonist (EC50 = 40 nM by GTPγS binding assay; IC50 = 0.28 nM against 1 μM forskolin-stimulated cellular cAMP accumulation) with good selectivity over opioid receptors μ, k, δ (Ki = 5.9, 26, 250 nM against 1.5 nM naloxone, 3 nM naloxone, 0.3 nM [Ile5,6]-deltorphin II for binding respective receptors), dopamine and serotonin receptors (Ki = 520 nM/D2, 1210 nM/D3,350 nM/D4.4; Ki ≥1 μM for 5HT 1Dα, 2A, 2C, 6, 7). Ro 65-6570 elicits ORL1-dependent anxiolytic-like effects in rats in vivo (0.32-3.2 mg/kg i.p.; elevated plus maze) without affecting spontaneous locomotion. Unlike OFQ, Ro 65-6570 does not affect cocaine-induced conditioned place preference (CPP) in rats.

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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S Röver et al.
Journal of medicinal chemistry, 43(7), 1329-1338 (2001-02-07)
The discovery of 8-(5,8-dichloro-1,2,3,4-tetrahydro-naphthalen-2-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one, 1a, as a high-affinity ligand for the human ORL1 (orphanin FQ/nociceptin) receptor led to the synthesis of a series of optimized ligands. These compounds exhibit high affinity for the human ORL1 receptor, exhibit moderate to good
L Asth et al.
Neuropharmacology, 105, 434-442 (2016-02-13)
Nociceptin/orphanin FQ (N/OFQ) receptor (NOP) agonists produce anxiolytic-like effects in rodents while antagonists promote antidepressant-like effects. The aim of this study was to investigate the effect on anxiety and depression of NOP receptor partial agonists such as the peptides [F/G]N/OFQ(1-13)NH2
Anna Rizzi et al.
Pharmacology research & perspectives, 4(4), e00247-e00247 (2017-01-25)
The aim of the study was to investigate the in vitro and in vivo pharmacological profile of cebranopadol, a novel agonist for opioid and nociceptin/orphanin FQ (N/OFQ) receptors (NOP). In vitro cebranopadol was assayed in calcium mobilization studies in cells coexpressing NOP
Khaoula Rekik et al.
Neuropharmacology, 125, 39-49 (2017-07-15)
Several neuropeptidergic systems act as modulators of cognitive performances. Among them, nociceptin, an opioid-like peptide also known as orphanin FQ (N/OFQ), has recently gained attention. Stimulation of its receptor, the N/OFQ opioid receptor (NOP), which is expressed in brain regions
A Rizzi et al.
Peptides, 94, 71-77 (2017-07-13)
Nociceptin/orphanin FQ (N/OFQ) modulates several biological functions, including pain transmission via selective activation of a specific receptor named NOP. The aim of this study was the investigation of the antinociceptive properties of NOP agonists and their interaction with opioids in
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